Cat. No. 1990
Chemical Name: (R,R)-5,11-Diethyl-5,6,11,12-tetrah
Biological ActivityNon-steroidal, selective estrogen receptor ligand; agonist at ERα receptor (Ki = 9.0 nM) and antagonist at ERβ receptor (Ki = 3.6 nM).
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Kraichely et al (2000) Conformational changes and coactivator recruitment by novel ligands for estrogen receptor-α and estrogen receptor-β: correlations with biological character and distinct differences among SRC coactivator family members. Endocrinology 141 3534. PMID: 11014206.
Sun et al (1999) Novel ligands that function as selective estrogens or antiestrogens for estrogen receptor-α or estrogen receptor-β. Endocrinology 140 800. PMID: 9927308.
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Citations are publications that use Tocris products. Selected citations for (R,R)-THC include:
Nicholson et al (2015) Estrogen receptor-α is a key mediator and therapeutic target for bladder complications of benign prostatic hyperplasia. PLoS One 193 722. PMID: 25167991.
Wang et al (2015) Bu-Shen-Ning-Xin decoction: inhibition of osteoclastogenesis by abrogation of the RANKL-induced NFATc1 and NF-κB signaling pathways via selective estrogen receptor α. Drug Des Devel Ther 9 3755. PMID: 26229438.
Simpkins et al (2012) Src Inhibition with saracatinib reverses fulvestrant resistance in ER-positive ovarian cancer models in vitro and in vivo. Clin Cancer Res 18 5911. PMID: 22896656.
Xing et al (2012) Estrogen modulates NFκB signaling by enhancing IκBα levels and blocking p65 binding at the promoters of inflammatory genes via estrogen receptor-β. PLoS One 7 e36890. PMID: 22723832.
Guo et al (2011) Baicalin, a flavone, induces the differentiation of cultured osteoblasts: an action via the Wnt/beta-catenin signaling pathway. J Biol Chem 286 27882. PMID: 21652696.
Kola et al The orexigenic effect of ghrelin is mediated through central activation of the endogenous cannabinoid system. PLoS One 3 e1797. PMID: 18335063.
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Keywords: (R,R)-THC, supplier, Potent, subtype, selective, ligands, Erα, Eralpha, agonists, ERβ, ERbeta, antagonists, ER, ERR, Estrogen, Receptors, Tocris Bioscience, Estrogen and Related Receptor products
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